The small molecule dorsomorphin, also known as compound C, is a cell-permeable pyrazolopyrimidine derivative, which acts as a potent and reversible ATP-competitive inhibitor of AMP-activated protein kinase (AMPK). Recent studies indicated that several molecules with functions in other signaling pathways, including bone morphogenetic protein (BMP) signaling, are novel targets of dorsomorphin. This report focuses on two major targets of dorsomorphin and provides insight into the use of dorsomorphin in the analysis of intracellular signaling.